Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.
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Calcitriol Chemical Structure
CAS No. : 32222-06-3
This product is a controlled substance and not for sale in your territory.
Based on 46 publication(s) in Google Scholar
Other Forms of Calcitriol:
Calcitriol Derivatives
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Calcitriol-d6
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(1S)-Calcitriol
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Calcitriol-13C3
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Calcitriol-d3
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Calcitriol-13C5
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Calcitriol (Standard)
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Calcitriol purchased from MedChemExpress. Usage Cited in:
Int Immunopharmacol. 2017 Jun;47:182-189.
[Abstract]
The total number of sneezing and nasal rubbing motions is significantly reduced by 1,25-(OH)2D3, n=9.
Calcitriol purchased from MedChemExpress. Usage Cited in:
Oncotarget. 2017 Oct 26;8(59):100187-100195.
[Abstract]
Calcitriol increases the expressions of JMJD3 and p16INK4A. 786-O cells are treated with vehicle (Veh) or 100nM Calcitriol (Cal) for 48h, and untreated group as control (Con). The expressions of JMJD3 and p16INK4A are determined with western blotting.
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Description
Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.
IC50 & Target
Human Endogenous Metabolite
In Vitro
Calcitriol exerts antiproliferative effects on cervical cancer cells in vitro. Cells decrease by 12.8% when treated with 100 nM Calcitriol for 6 days, compare with control. Inhibition of cell proliferation becomes more pronounced with the increase in Calcitriol concentration. The decrease is 26.1% and 31.6% for 200 and 500 nM Calcitriol, respectively. Treatment with Calcitriol for 72 h induces an evident accumulation of cells in the G1 phase, with approximately 66.18% in 200 nM and 78.10% in 500 nM, compare with the control (24.36%). Calcitriol treatment significantly decreases HCCR-1 protein expression compare with the control in a time- and dose-dependent manner[1]. Calcitriol significantly increases ERα mRNA in a dose dependent manner with an EC50 of 9.8×10-9 M[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Calcitriol Related Antibodies
In Vivo
Chronic treatment with Calcitriol (150 ng/kg per day for 4.5 months) improves the relaxations (pD2: 6.30±0.09, Emax: 68.6±3.9% in Calcitriol-treated OVX, n=8). Renal blood flow in OVX rats is reduced in both kidneys, and the flow is restored by Calcitriol treatment. The increased expression of COX-2 and Thromboxane-prostanoid (TP) receptor in OVX rat renal arteries is reduced by chronic calcitriol administration[3]. High- and low-dose Calcitriol treatment significantly decreases the systolic blood pressure (SBP) in the fructose-fed rats by 14±4 and 9±4 mmHg, respectively, at Day 56. High-dose Calcitriol treatment (20 ng/kg per day) significantly increases serum ionized calcium level (1.44±0.05 mmol/L) compare with the other groups[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, protect from light, stored under nitrogen
*The compound is unstable in solutions, freshly prepared is recommended.
Solvent & Solubility
In Vitro:
DMSO : 110 mg/mL (264.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 100 mg/mL (240.02 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.4002 mL
12.0009 mL
24.0017 mL
5 mM
0.4800 mL
2.4002 mL
4.8003 mL
10 mM
0.2400 mL
1.2001 mL
2.4002 mL
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Solubility: 2.75 mg/mL (6.60 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (27.5 mg/mL) to 900 μLCorn oil, and mix evenly.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 7
Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 8
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
Solubility: 0.55 mg/mL (1.32 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
*The compound is unstable in solutions, freshly prepared is recommended.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Wang G, et al. Calcitriol Inhibits Cervical Cancer Cell Proliferation Through Downregulation of HCCR1 Expression. Oncol Res. 2014;22(5-6):301-9.
[Content Brief]
[2]. Santos-Martínez N, et al. Calcitriol restores antiestrogen responsiveness in estrogen receptor negative breast cancer cells: a potential new therapeutic approach. BMC Cancer. 2014 Mar 29;14:230.
[Content Brief]
[3]. Dong J, et al. Calcitriol restores renovascular function in estrogen-deficient rats through downregulation of cyclooxygenase-2 and the thromboxane-prostanoid receptor. Kidney Int. 2013 Jul;84(1):54-63.
[Content Brief]
[4]. Chou CL, et al. Beneficial effects of calcitriol on hypertension, glucose intolerance, impairment of endothelium-dependent vascular relaxation, and visceral adiposity in fructose-fed hypertensive rats. PLoS One. 2015 Mar 16;10(3):e0119843.
[Content Brief]
Cell Assay
[1]
HeLa S3 cells are plated at a density of 1,000 cells/well in 96-well plates of Dulbecco’s modified Eagle’s medium (DMEM) with 10% fetal bovine serum (FBS), treated with 1% ethanol (control) or various concentrations of Calcitriol (100, 200, and 500 nM) for 72 h. A Cell Counting Kit8 (CCK-8) is used to determine cell proliferation. At 24, 48, 72, 96, 120, and 144 h after culturing with 200 nM Calcitriol, cells are harvested for analysis. Three independent experiments are performed in quadruplicate[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]
Adult female Sprague-Dawley rats weighing 200 to 220g are used in this study. Rats are housed in a temperature-controlled room (~23°C) with a 12-h light/dark cycle. The animals have free access to a standard diet and water. Ovariectomy (OVX) is performed on rats. At 6 months after the surgical procedure, the OVX rats are randomly assigned to either treatment with vehicle dimethyl sulfoxide (OVX+vehicle) or Calcitriol (150 ng/kg daily, OVX+calcitriol). Calcitriol treatment is given by oral gavage and lasted or 4.5 months. Blood pressure and serum Calcitriol level are measured[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
[1]. Wang G, et al. Calcitriol Inhibits Cervical Cancer Cell Proliferation Through Downregulation of HCCR1 Expression. Oncol Res. 2014;22(5-6):301-9.
[Content Brief]
[2]. Santos-Martínez N, et al. Calcitriol restores antiestrogen responsiveness in estrogen receptor negative breast cancer cells: a potential new therapeutic approach. BMC Cancer. 2014 Mar 29;14:230.
[Content Brief]
[3]. Dong J, et al. Calcitriol restores renovascular function in estrogen-deficient rats through downregulation of cyclooxygenase-2 and the thromboxane-prostanoid receptor. Kidney Int. 2013 Jul;84(1):54-63.
[Content Brief]
[4]. Chou CL, et al. Beneficial effects of calcitriol on hypertension, glucose intolerance, impairment of endothelium-dependent vascular relaxation, and visceral adiposity in fructose-fed hypertensive rats. PLoS One. 2015 Mar 16;10(3):e0119843.
[Content Brief]
[1]. Wang G, et al. Calcitriol Inhibits Cervical Cancer Cell Proliferation Through Downregulation of HCCR1 Expression. Oncol Res. 2014;22(5-6):301-9.
[2]. Santos-Martínez N, et al. Calcitriol restores antiestrogen responsiveness in estrogen receptor negative breast cancer cells: a potential new therapeutic approach. BMC Cancer. 2014 Mar 29;14:230.
[3]. Dong J, et al. Calcitriol restores renovascular function in estrogen-deficient rats through downregulation of cyclooxygenase-2 and the thromboxane-prostanoid receptor. Kidney Int. 2013 Jul;84(1):54-63.
[4]. Chou CL, et al. Beneficial effects of calcitriol on hypertension, glucose intolerance, impairment of endothelium-dependent vascular relaxation, and visceral adiposity in fructose-fed hypertensive rats. PLoS One. 2015 Mar 16;10(3):e0119843.
Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
Ethanol / DMSO
1 mM
2.4002 mL
12.0009 mL
24.0017 mL
60.0043 mL
5 mM
0.4800 mL
2.4002 mL
4.8003 mL
12.0009 mL
10 mM
0.2400 mL
1.2001 mL
2.4002 mL
6.0004 mL
15 mM
0.1600 mL
0.8001 mL
1.6001 mL
4.0003 mL
20 mM
0.1200 mL
0.6000 mL
1.2001 mL
3.0002 mL
25 mM
0.0960 mL
0.4800 mL
0.9601 mL
2.4002 mL
30 mM
0.0800 mL
0.4000 mL
0.8001 mL
2.0001 mL
40 mM
0.0600 mL
0.3000 mL
0.6000 mL
1.5001 mL
50 mM
0.0480 mL
0.2400 mL
0.4800 mL
1.2001 mL
60 mM
0.0400 mL
0.2000 mL
0.4000 mL
1.0001 mL
80 mM
0.0300 mL
0.1500 mL
0.3000 mL
0.7501 mL
100 mM
0.0240 mL
0.1200 mL
0.2400 mL
0.6000 mL
Calcitriol Related Classifications
Cancer
Cancer Targeted TherapyCancer Metabolism and Metastasis
Vitamin D Related/Nuclear ReceptorMetabolic Enzyme/Protease
Drug MetaboliteVD/VDREndogenous Metabolite
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
Calcitriol32222-06-31,25-Dihydroxyvitamin D3Drug MetaboliteVD/VDREndogenous MetaboliteVitamin DVitamin D receptorInhibitorinhibitorinhibit
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